BRD3731 is a Selective GSK3β Inhibitor

Glycogen synthase kinase 3 (GSK3) is a key regulatory kinase in the WNT pathway. GSK3 remains a therapeutic target of interest in many diseases. GSK3 represents an example of such an evolutionary selection system, resulting in two paralog genes, GSK3A on chromosome 19 and GSK3B on chromosome 3. The...

Mavelertinib is a Selective and Irreversible EGFR TKI

Mutant EGFRs are one of the major drivers of non-small-cell lung cancer (NSCLC). While reversible first-generation EGFR inhibitors are initially an effective treatment. However, a drug-resistant gatekeeper T790M mutation accounts for ∼50% of disease progression in patients with first-generation agents. Irreversible second-generation EGFR inhibitors are more potent against the...

NEO2734 is an Orally Active Dual p300/CBP and BET Bromodomain Selective Inhibitor

NUT midline carcinoma (NMC) is a rare, aggressive subtype of squamous carcinoma. This kind of cancer is usually driven by BRD4-NUT fusion oncoprotein. BRD4, a BET protein, binds to chromatin through its two bromodomains. At the same time, NUT recruits the p300 HAT to activate oncogenic target genes transcription....

Giredestrant is an Orally Active and Selective ER Antagonist

Estrogen receptor (ERs) is a group of proteins found in cells and is activated by estrogen. Specifically, ERs are typical members of the nuclear receptor superfamily, including receptors that mediate steroid hormones, thyroid hormones, vitamin A and vitamin D, and many orphan receptors. Besides, once ER is activated, estrogen...

D-3263 is a TRPM8 Agonist with Potential Antineoplastic Activity

The transient receptor potential melastatin (TRPM) family is a part of the TRP protein superfamily. TRP protein superfamily contains TRPM1 to TRPM8 and involves various processes including temperature sensing, ion homeostasis, and redox sensing. Transient receptor potential melastatin (TRPM) ion channels play an important role in many physiological processes....

CMLD012612 is a Potent Eukaryotic Initiation Factor 4A (eIF4A) Inhibitor

Small molecules show targeting the translation machinery that can be used for the research of cancer, viral infection, and neurodegeneration. In particular, a class of translation inhibitors that possess potent cytotoxic activity against tumor cells is in the development. In this article, we will introduce a potent eukaryotic initiation...